KC7F2

Cat No.:V0299 Purity: ≥98%
KC7F2 is a novel and potent HIF-1 (hypoxia inducible factor-1) pathway inhibitor with potential anticancer activity.
KC7F2 Chemical Structure CAS No.: 927822-86-4
Product category: HIF
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
KC7F2 is a novel and potent HIF-1 (hypoxia inducible factor-1) pathway inhibitor with potential anticancer activity. KC7F2 is cytotoxic agent to a variety of cancer cell lines with an IC50 value of 15-25 µM. KC7F2 markedly inhibited HIF-mediated transcription in cells derived from different tumor types, including glioma, breast, and prostate cancers, and exhibited enhanced cytotoxicity under hypoxia. KC7F2 prevented the activation of HIF-target genes such as carbonic anhydrase IX, matrix metalloproteinase 2, endothelin 1, and enolase 1.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
KC7F2 (0-80 μM; 6 hours) potently reduces HIF-1α protein levels in a dose-dependent manner under hypoxic conditions; HIF-1α levels were significantly reduced at a concentration of 20 μM [Conditions [1]. KC7F2 (15-25 μM; 0-72 hours) exhibits clear dose-responsive cytotoxicity with IC50 values of approximately 15-25 μM, depending on the cell line, and this effect is more severe under hypoxic conditions. The rate at which HIF-1α protein regulation occurs is unaffected by KC7F2 [1]. While HIF-1α mRNA regulation is not inhibited by KC7F2, its protein production is [1]. The eukaryotic initiation regulator 4E-binding protein 1 (4EBP1) is regulated by KC7F2 [1]. Cell
Cell Assay
Cell cytotoxicity assay [1]
Cell Types: MCF7 cells, LNZ308 cells, A549 cells, U251MG cells, LN229 cells
Tested Concentrations: 15–25 μM
Incubation Duration: 0-72 hrs (hours)
Experimental Results: Cytotoxicity is more obvious in tumors phosphorylated [1]. Cell lines compared to normal cells.

Cell viability assay[1]
Cell Types: LN229 Cell
Tested Concentrations: 6 hrs (hours)
Incubation Duration: 0 μM, 5 μM, 7.5 μM, 10 μM, 15 μM, 20 μM, 30 μM, 40 μM, 60 μM, 80 μM
Experimental Results: Reduction HIF-1α protein levels were dose-dependent.
References
[1]. Narita T, et al. Identification of a novel small molecule HIF-1alpha translation inhibitor. Clin Cancer Res. 2009 Oct 1;15(19):6128-6136.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H16CL4N2O4S4
Molecular Weight
570.38
CAS #
927822-86-4
SMILES
ClC1C([H])=C([H])C(=C([H])C=1S(N([H])C([H])([H])C([H])([H])SSC([H])([H])C([H])([H])N([H])S(C1C([H])=C(C([H])=C([H])C=1Cl)Cl)(=O)=O)(=O)=O)Cl
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 32 mg/mL (~56.10 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.5 mg/mL (4.38 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7532 mL 8.7661 mL 17.5322 mL
5 mM 0.3506 mL 1.7532 mL 3.5064 mL
10 mM 0.1753 mL 0.8766 mL 1.7532 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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